Brassicaceae are widely consumed in many parts of the world and their dietary intake has been associated with cancer risk reduction. Extracts and metabolites derived from cruciferous vegetables have thus gained popularity as potential cancer chemopreventive agents. We have previously found, unexpectly, that glucoraphanin, the most extensively present glucosinolate in these vegetables, is a potent mutagen bioactivating Phase-I enzyme inducer. In the present study, the influence of black cabbage seed extract, rich in glucoraphanin, was investigated on Phase-I enzymes in different organs of male or female rats. Oral seed extract injection at 120 or 240 mg/kg b.w. for one or four consecutive days, significantly affected various cytochrome P450 (CYP) -linked monooxygenases in a complex way being the lung the most responsive organ (in males, up to ∼2600% increase for CYP2B1/2 isoform and ∼96% loss for CYP1A1, CYP3A1/2). These findings indicate that the extract may strongly enhance and/or suppress rat xenobiotic biotransformation pathways and that caution should be paid to the possible influence on human metabolism. These data suggest an overall evaluation of the balance between beneficial vs. possible adverse effects for each agent, even if of natural origin, prior to routinely, preventive mass use.
Aim of the study: The multiple sclerosis is an immuno-mediated disorder of the Central Nervous System characterized by inflammatory processes and neurodegenerative changes. It has been shown that the endocannabinoid system is altered in this disease and that the exogenous cannabinoids may play a possible role in its therapeutic management. The aim of the present study was to investigate the efficacy of crude extracts of Cannabis sativa on motor symptoms in the chronic relapsing experimental autoimmune encephalomyelitis (CREAE), a murine model of multiple sclerosis.Materials and methods: CREAE-induced mice were injected by different crude ethanolic extracts from Cannabis sativa, containing Delta(9)-tetrahydrocannabinol, cannabidiol, or cannabinoid-free, respectively. The effect of the combined treatment with Delta(9)-tetrahydrocannabinol and cannabidiol extracts has also been investigated. All extracts were administered in acute and chronic experimental protocols.Results: The chronic administration of Delta(9)-tetrahydrocannabinol-rich extract resulted in a significant reduction of neurological deficits that lasted until the end of the observations. The acute and chronic treatments with the cannabidiol-rich extract resulted unable to induce changes of neurological signs. However, during the relapse phase a significant decrease of neurological scores was observed. The combined treatment with Delta(9)-tetrahydrocannabinol and cannabidiol extracts was ineffective, whereas the acute administration of the cannabinoid-free extract showed a significant improvement.Conclusions: Our study shows a patchy effect of different cannabinoid extracts on CREAE-induced motor deficits. Although the effect of crude extracts of Cannabis sativa here reported need to be further investigated to define the exact therapeutic target of each cannabinoid, it may represent a possible therapeutic approach for the management of the multiple sclerosis. (C) 2010 Elsevier Ireland Ltd. All rights reserved.
Laurus nobilis L. (Family Lauraceae) is an evergreen tree widely distributed in the Mediterranean area and Europe. It is used in folk medicine of different countries as a stomachic and carminative as well as in treatment of gastric diseases. Extracts obtained with different methods (methanol and chloroform) from laurel leaves were evaluated for their gastroprotective activities in the rat. The antioxidant capacity of the different extracts has been also measured in vitro. In order to confirm the activities investigated, histological observations were performed. The gastric damage was significantly reduced by all extracts administered. The more effective protection was produced by chloroformic and methanolic crude extracts. The results obtained after oral administration of L. nobilis leaf extracts are in good agreement with their antioxidant capacity, confirming the relationship between pharmacological efficacy and antiradical activity. Histological evidences confirm the results evaluated with the animal procedures.
Ethnopharmacological relevance: Rosa canina L is a medicinal plant largely used in traditional folk medicine. Several compounds from rose hip extracts were reported to display in vitro anti-inflammatory activities.Aim of the study: The in vivo effects of Rosa canina extracts are still poorly investigated. In the present study the anti-inflammatory and the gastroprotective effects of a hydroalcoholic crude extract of Rosa canina fruits were tested in rat.Materials and methods: The anti-inflammatory activity of the extract was tested on the carrageenin-induced rat paw edema assay. The gastroprotective effect was investigated on the ethanol-induced gastric damage model. The in vitro antioxidant activity of this extract was also quantified using the Briggs-Rauscher oscillating reaction, the Trolox Equivalent Antioxidant Capacity method, and the Total Phenolic Content.Results: Data show that the Rosa canina extract inhibits the development of carrageenin-induced edema; the anti-inflammatory power is similar to that of indomethacin. The antiedema effect was more significant using a higher dose of the extract. The total score expressing gastric damage was lower in Rosa canina pre-treated stomachs with respect to unpre-treated ones, although the antiulcerogenic effectiveness was not statistically significant. The antiulcerogenic effectiveness was not statistically detectable, even if the total score expressing gastric damage was lower in Rosa canina stomachs from pre-treated rats with respect to unpre-treated ones. Chemical analysis revealed that the extract owns a good antioxidant activity that may also contribute to the anti-inflammatory effects observed in vivo.Conclusions: Altogether, the present data demonstrate the anti-inflammatory property of Rosa canina suggesting its potential role as adjuvant therapeutic tool for the management of inflammatory-related diseases. (C) 2011 Elsevier Ireland Ltd. All rights reserved.
Oxidative stress is reported to be closely related to pathogenetic mechanisms and plays a central role in several molecular toxicities. It seems reasonable to hypothesize that antioxidant molecules and/or free radical scavengers can protect from oxidative stress-induced damage by quenching free-radical reactions. Leontopodic acid (LA) is a fully substituted, hexaric acid derivative isolated from Leontopodium alpinum Cass., commonly known as ‘Edelweiss’ (Asteraceae family), and exhibits significant chemical antioxidant power. The present study was designed to evaluate LA’s capacity to counteract induced oxidative stress in two in vitro cell models: one exposed the LLC-PK1 cell line to ochratoxin A and the other exposed the differentiated SH-SY5Y cells to amyloid β. The effects of a 24 h pretreatment with LA on induced ROS (reactive oxygen species) production and cytotoxicity were evaluated in the two models. Surprisingly, the results showed that while LA decreased ROS production, it did not increase cell survival.
Several in vitro studies showed that free radical scavengers possess chemopreventive properties against mycotoxin‐induced cell damage which are at least partially associated with the induction of phase II detoxifying enzymes and antioxidant enzymes like glutathione S ‐transferase (GST) and glutathione peroxidase (GPx). The aim of this project was to study the chemopreventive effects of leontopodic acid (LA), a potent natural occurring free radical scavenger isolated from the aerial parts of Leontopodium alpinum . Different mycotoxins were evaluated in two different cell lines on the basis of their specific toxicity: aflatoxin B1 (AFB1) on HepG2 cells and deoxynivalenol (DON) on U937 cells. Cell viability and reactive oxygen species concentration were determined, and the effects of pre‐treatment with LA on these parameters were investigated together with the GST and GPx activity as well as the concentration of reduced glutathione. The results show that LA protects U937 cells from DON‐induced cell damage but not HepG2 cells from AFB1. Moreover LA is able to enhance GPx activity in U937, but not GST activity in HepG2. We hypothesize that the increase in detoxifying enzymes is probably the main mechanism of antioxidant mediated chemoprevention. Copyright © 2008 John Wiley & Sons, Ltd.
Laurus nobilis L. (laurel) leaves are frequently used as a spice for cooking purposes. Folk medicine in many countries uses the infusion of the plant in stomachic and carminative remedies, as well as for the treatment of gastric diseases. Little information is available about the phytochemical composition of the infusion of dried leaves, which is a way to consume this aromatic and medicinal plant. Phytochemical investigations on the infusion were performed by high-performance liquid chromatography (HPLC) with a diode array detector (DAD) and direct electrospray ionization-tandem mass spectrometry. Several flavonoid derivatives were detected. Semipreparative HPLC from the infusion of laurel leaves isolated 10 flavonoid O-glycosides, one flavonoid C-glycoside, catechin, and cinnamtannin B1. Structures of the isolated compounds were computed on the basis of spectral measurements including high-resolution mass spectrometry spectroscopy and one- and two-dimensional nuclear magnetic resonance techniques. The amount of the flavonoids was also determined by HPLC-DAD. The antioxidant activity of the tea and the isolated compounds was also measured using two different in vitro methods: the Briggs-Rauscher oscillating reaction test, at a pH similar to that of the gastric juice, and the Trolox equivalent antioxidant capacity assay, at the pH of blood. For the infusion and the methanol extract the total phenolic content was also measured using the Folin-Ciocalteu reagent.
Laurus nobilis L. (laurel) leaves are frequently used as a spice for cooking purposes. Folk medicine in many countries uses the infusion of the plant in stomachic and carminative remedies, as well as for the treatment of gastric diseases. Little information is available about the phytochemical composition of the infusion of dried leaves, which is a way to consume this aromatic and medicinal plant. Phytochemical investigations on the infusion were performed by high-performance liquid chromatography (HPLC) with a diode array detector (DAD) and direct electrospray ionization-tandem mass spectrometry. Several flavonoid derivatives were detected. Semipreparative HPLC from the infusion of laurel leaves isolated 10 flavonoid O-glycosides, one flavonoid C-glycoside, catechin, and cinnamtannin B1. Structures of the isolated compounds were computed on the basis of spectral measurements including high-resolution mass spectrometry spectroscopy and one- and two-dimensional nuclear magnetic resonance techniques. The amount of the flavonoids was also determined by HPLC-DAD. The antioxidant activity of the tea and the isolated compounds was also measured using two different in vitro methods: the Briggs-Rauscher oscillating reaction test, at a pH similar to that of the gastric juice, and the Trolox equivalent antioxidant capacity assay, at the pH of blood. For the infusion and the methanol extract the total phenolic content was also measured using the Folin-Ciocalteu reagent.
Mycotoxins are secondary metabolites of various moulds that contaminate several alimentary substrates. One of the most dangerous of these is ochratoxin A (OTA). Reactive oxygen species (ROS) play an important role in the toxicity mechanism of OTA, so the use of natural or synthetic free radical scavengers could be a potential chemopreventive strategy. Carnosic acid (CA) is the major polyphenolic compound present in rosemary plants. This work aimed to determine whether CA could counteract OTA-induced cell damage. Free radical scavenging properties of CA were chemically determined at pH 7.4. Cytotoxicity of CA and OTA on LLC-PK1 cells, and the protective effects of CA, were assessed using the Alamar Blue test. The effects in vitro of CA pre-treatment on the production of ROS, the DNA oxidation and the induction of apoptosis induced by OTA were studied. It was found that CA has free radical scavenging properties at both the considered pH values. Moreover, a pre-treatment of 24 h with 10, 20 and 30 µM CA is able to reduce OTA-induced cytotoxicity; a pre-treatment of 24 h with 20 and 30 µM CA achieved ROS reduction and with 30 µM CA decreased the OTA-induced increase of 8-OH-2'-deoxyguanosine and of DNA fragmentation in LLC-PK1. These findings suggest a starting point to develop alimentary strategies against OTAinduced cell damage. Moreover, our results provide further evidence that oxidative stress plays an important role in the OTA cytotoxicity mechanism.
Summary The antioxidant capacities and the total phenolic content in cocoa liquor directly manufactured chocolate from an artisan manufacturer were measured using different in vitro methods (BR, TEAC, and Folin–Ciocalteu Reagent). These parameters were then compared with those of a chocolate made by a leading manufacturing company producing chocolate and cocoa‐containing products. A statistical analysis of the collected data showed that the antioxidant properties of the artisan‐made chocolate are significantly better than those of the factory‐produced one. These results were ascribed to the fact that all the bioactive components in the cocoa beans are better preserved in the artisan‐made chocolate.
According to folk medicine some species belonging to the genus Cyclamen were used for their biological activities. Early investigation of the different species of the genus resulted in the isolation of triterpenic saponins. No phytochemical and biological data are available on C. repandum. As part of a series of phytochemical investigations for bioactive compounds from medicinal plants, Cyclamen repandum S. et S. was investigated. The present study sought to find the antiinflammatory and antinociceptive activities of C. repandum tubers in rats and mice. A preliminary screening was conducted with three different extracts in the tests used, particularly the paw edema and the writhing tests. Subsequently some saponins isolated from the ME extract, the more effective one, have been identified. This paper also describes the results of fractionation and bioassay guided chemical studies. Chemical investigation of the active extract afforded the isolation and characterization of six triterpenic saponins. The possible antiinflammatory and analgesic properties were investigated as the saponin content of the fractions allows to speculate on such aspect.
Verbena officinalis L. is used in folk medicine for the treatment of inflammatory disorders, skin burns, abrasions, and gastric diseases. Extracts obtained with different solvents (methanol, VoME; enriched flavonoids, VoEF; supercritical CO2, VoCO2) were evaluated for anti-inflammatory, gastroprotective and cicatrizing activities. Additionally, the antioxidant capacity was determined in vitro. In order to confirm the activities investigated, histological observations were performed. All extracts induce a remarkable anti-inflammatory activity. The gastric damage is significantly reduced by all extracts administered, whereby the most pronounced protection is observed for the VoCO2 and VoEF extracts. Finally, a wound healing effect is obtained particularly by the CO2 extract, suggesting the presence of some lipophilic active principles. Histological evidence confirms the results evaluated with the animal procedures. The results obtained after oral administration of V. officinalis extracts are also in agreement with the antioxidant capacity evaluated in vitro, confirming the relationship between pharmacological activities and antiradical efficacy.
Besides aflatoxin B1, recent findings suggested that oxidative stress plays an important role in the toxicity of an other mycotoxin: ochratoxin A (OTA). The protective effect of two catechins (epigallocatechin gallate, EGCG, and epicatechin gallate, ECG) against OTA-induced cytotoxicity was investigated in a pig kidney cell line (LLC-PK1). The ability of the catechins to reduce ROS production and DNA fragmentation induced by OTA was also investigated. Our experiments proved the significant cytoprotective effects of the molecules in vitro from OTA-induced cell damage. In particular a 24 h pre-treatment with EGCG or ECG restored cell viability with respect to OTA alone. Pre-treatment with EGCG at low concentration for 8 days protected cells from OTA-induced cell death. Moreover both catechins reduced OTA-induced ROS production. A reduction of OTA-induced DNA fragmentation was found for LLC-PK1 cells pre-treated with EGCG and ECG. The free-radical scavenging capacity of both catechins was tested with the Briggs–Rauscher oscillating method (pH ≈ 2) and the TEAC assay (pH 7.4). The results show a good scavenging power according with inhibition of ROS production. Catechins could be useful to develop alimentary strategies for both humans and animals to prevent OTA-induced cytotoxicity.
Brassica vegetables and glucosinolates contained therein are supposed to reduce the risk of cancer and to possess health-promoting properties. The benefits of a Brassica-based diet may be particularly expressed by eating sprouts, in which the glucosinolate content is higher than in mature vegetables. With this in mind, a first objective of this study was to evaluate the antioxidant properties of radish (Raphanus sativus L.) sprouts (Kaiware Daikon) extract (KDE), in which the glucosinolate glucoraphasatin (GRH), showing some antioxidant activity, is present at 10.5% w/w. The contribution of GRH to KDE's antioxidant activity was considered in two chemical assays (Trolox equivalent antioxidant capacity and Briggs-Rauscher methods). The total phenol assay by Folin-Ciocalteu reagent was performed to quantify the reducing capacity of KDE. Finally, on the basis of the putative choleretic properties of antioxidant plant extracts, the effect on the bile flow of KDE administration was investigated in an animal experimental model. The findings showed that KDE has antioxidant properties and significantly induced bile flow in rats administered 1.5 g/kg of body weight for 4 consecutive days.
Dichloromethane, methanolic and CO(2) extracts of the aerial parts and roots of Edelweiss (Leontopodium alpinum Cass.) were investigated for their anti-inflammatory and analgesic effects after oral administration. The highest activity in rat's paw edema assay was found for the lipophilic extracts of the aerial plant parts (dose 200 mg/kg), exhibiting a swelling reduction of 72% (CO(2)-extract) and 80% (DCM-extract), respectively. Histological evaluation of the treated paws showed a significant reduction of the inflammatory response in the pre-treated specimens. On the contrary in the acetic acid-induced writhing test the dichloromethane extract of the root extract exhibited more pronounced analgesic effects than the extracts of the aerial parts, suggesting a different pattern of active compounds. As far as gastrointestinal effects are concerned, oral administration of aerial parts (hDCM 200 mg/kg) to mice induces a highly significant inhibition in gastrointestinal propulsion probably related to the presence of so far unknown compounds. Moreover, the antioxidant capacity of some extracts was studied in order to establish a possible correlation with anti-inflammatory properties.
Since oxidative stress plays an important role in the toxicity mechanism of several mycotoxins such as affatoxin B1 (AFB1), the use of natural or synthetic free radical scavengers could be a potential chemopreventive strategy.Carnosic acid (CA) is the major polyphenolic compound present in rosemary plants and it can also be found in sage leaves. Its free radical scavenging properties were tested with two chemical methods. It was found that it has good free radical scavenging capacity at pH 7.4.This study also found that a 24 h pre-treatment with 10, 20 and 30 mu m CA led to a clear, dose-dependent protective effect on cell toxicity, reducing cell death induced by a 24 h exposure with 10 mu m AFB1, respectively, by 16% (P < 0.05), 26% (P < 0.01) and 63% (P < 0.001). It was also found that a 24 h pre-treatment with 20 and 30 mu m CA achieved a reduction of ROS levels, respectively, of 146% (P < 0.001) and 173% (P < 0.001) in HepG2 cells exposed to 10 mu m AFB1 for 8 h. Moreover, in cells pre-incubated with 30 mu m CA for 24 h the concentration of 8-OH-deoxyguanine decreased by 57% (P < 0.001) with respect to the cells exposed for 24 h to 10 mu m AFB1 alone.The results obtained with the in vitro and chemical studies support the theory that AFB1 induced oxidative stress plays an important role in the cytotoxic mechanism of this mycotoxin. Furthermore these findings suggest a starting point for developing alimentary strategies in order to counteract the damage caused by AFB1 contamination in feed and food. Copyright (c) 2006 John Wiley & Sons, Ltd.